Design, synthesis and biological evaluation of novel hamamelitannin analogues as potentiators for vancomycin in the treatment of biofilm related Staphylococcus aureus infections
Design, synthesis and biological evaluation of novel hamamelitannin analogues as potentiators for vancomycin in the treatment of biofilm related Staphylococcus aureus infections
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DOI：
10.1016/j.bmc.2016.07.058
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发表时间：
2016-10-01
影响因子：
3.5
通讯作者：
Van Calenbergh, Serge
中科院分区：
文献类型：
--
作者：
Vermote, Arno;Brackman, Gilles;Van Calenbergh, Serge
金黄色葡萄球菌是生物膜相关感染的常见原因。生物膜内的细菌细胞受到免疫系统的保护而不受攻击，常规抗生素通常无法穿透生物膜基质。金缕梅单宁作为抗生素增效剂的发现，最近导致了一个更像药物的铅的设计。在本研究中，我们希望进一步了解结构-活性关系（S.A.R.）通过制备21种金缕梅单宁类似物的文库，(C)2016爱思唯尔有限公司版权所有
Staphylococcus aureus is a frequent cause of biofilm-related infections. Bacterial cells within a biofilm are protected from attack by the immune system and conventional antibiotics often fail to penetrate the biofilm matrix. The discovery of hamamelitannin as a potentiator for antibiotics, recently led to the design of a more drug-like lead. In the present study, we want to gain further insight into the structure-activity relationship (S.A.R.) of the 5-position of the molecule, by preparing a library of 21 hamamelitannin analogues. (C) 2016 Elsevier Ltd. All rights reserved.